Bioorganic and Medicinal Chemistry p. 1597 - 1603 (1996)
Update date:2022-08-03
Topics:
Boger, Dale L.
Zhou, Jiacheng
The synthesis and evaluation of the analogues 3 and 4 of deoxybouvardin (1) and RA-VII (2), which contain modifications in the tetrapeptide subunit, are described. Unlike the natural products and similar to our prior disclosure, the agents 3 and 4, which substitute (Gly)4 and (Gly)3 for the D-Ala-Ala-NMe-Tyr(OMe)-Ala tetrapeptide subunit, exist in single rigid conformations in which the central cycloisodityrosine amide adopts its preferred trans stereochemistry and both were found to be biologically inactive.
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